PTP1B-IN-3

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PTP1B-IN-3 

PTP1B-IN-3 是有效的，有选择性的 PTP1B 抑制剂，对 PTP1B 和 TCPTP 的 IC50 值均为 120 nM。PTP1B-IN-3 具有抗糖尿病和抗癌作用。

PTP1B-IN-3

PTP1B-IN-3 Chemical Structure

CAS No. : 809272-64-8

规格 价格 是否有货
1 mg ￥8500 询问价格 & 货期
5 mg ￥25000 询问价格 & 货期
10 mg ￥44000 询问价格 & 货期

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PTP1B-IN-3 的其他形式现货产品:

PTP1B-IN-3 diammonium

生物活性

PTP1B-IN-3 is a potent and orally active PTP1B inhibitor with IC50s of 120 nM for both PTP1B and TCPTP. PTP1B-IN-3 has antidiabetic and anticancer effects[1][2].

IC50 & Target

IC50: 120 nM (PTP1B), 120 nM (TCPTP) [2]
体内研究
(In Vivo)

In diet-induced obese (DIO) mice, PTP1B-IN-3 (compounds 3g) exhibits dose dependent inhibition (60%, 80% and 100% inhibition at 1, 3 and 10 mg/kg, respectively) of glucose excursion when given orally 2 h before oral glucose challenge with an estimated ED50 of 0.8 mg/kg[1].
In the NDL2 Ptpn1 transgenic mice, PTP1B-IN-3 (compounds 3g; orally; 30 mg/kg for 21 days) shows a significant delay in the onset of tumor development in NDL2 Ptpn1+/+ mice, extending the median tumor free days (T50) from 28 days to 75 days[1].
In diet-induced obese (DIO) mice, PTP1B-IN-3 (compounds 3g) exhibits good oral bioavailability (F of 24%), slow clearance (CL of 0.71 mL/kg/min), and good elimination half live (t1/2 of 6 h). The oral bioavailability in higher species such as rats (F of 4%) and squirrel monkeys (F of 2%) are substantially lower but excellent exposures are achieved with oral dosing[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

362.06

Formula

C12H7BrF2NO3P
CAS 号

809272-64-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Yongxin Han, et al. Discovery of [(3-bromo-7-cyano-2-naphthyl)(difluoro)methyl]phosphonic acid, a potent and orally active small molecule PTP1B inhibitor. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3200-5.

    [2]. Patel D, .Discovery of orally active, potent, and selective benzotriazole-based PTP1B inhibitors. ChemMedChem. 2011 Jun 6; 6(6):1011-6.

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